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PubMed1987

Effects of the monobactam antibiotic aztreonam on platelet function and blood coagulation.

The effects of the new monobactam antibiotic aztreonam on platelet function and blood coagulation were evaluated both in vitro and ex vivo. In the in vitro studies carried out on platelets from 6 healthy volunteers, therapeutic concentrations of aztreonam had no effect on platelet function. Aztreonam inhibited platelet aggregation only at concentrations far in excess of those clinically achievable. In the ex vivo studies carried out in 11 patients with aztreonam-sensitive infections, aztreonam, 1 g t.i.d. intravenously, did not produce any effect on platelet function and blood coagulation. We conclude that therapeutic doses of aztreonam appear not to affect haemostasis.

Adenosine Diphosphate↗
PubMed1987

Comparative in vitro activity of carumonam (Ro 17-2301/AMA-1080), a new monobactam, and ceftriaxone against aerobic or facultative gram-negative isolates.

Carumonam (Ro 17-2301/AMA-1080) is a new monobactam antibiotic. A comparative in vitro evaluation with ceftriaxone was undertaken against 153 gram-negative clinical aerobic or facultative bacteria, both producers and nonproducers of beta-lactamase. Results indicated that carumonam had an enhancement of activity for Pseudomonas aeruginosa, Klebsiella oxytoca, Citrobacter freundii and Enterobacter cloacae and parallelled that of ceftriaxone against Escherichia coli, Klebsiella pneumoniae, Proteus spp. and Serratia marcescens. It can be concluded that carumonam could be an alternative of interest for the treatment of patients with infections due to gram-negative strains presumably or proven to be multiresistant.

Anti-Bacterial Agents↗
PubMed1989

Penetration of monobactam antibiotics (aztreonam, carumonam) into human prostatic tissue.

Concomitant concentrations of monobactam antibiotics were measured in plasma and in prostatic tissue obtained by transurethral resection in 25 patients, 60-120 min after dosage. A 1-gram single intravenous injection of aztreonam or carumonam yielded mean prostatic concentrations of 6.0 mg/kg in 20 patients. Five patients who received a 2-gram dose of carumonam demonstrated average prostatic levels of 10 mg/kg. These concentrations significantly exceed MIC values for most common gram-negative urinary tract pathogens.

Aged↗
PubMed1988

[The influence of a monobactam antibiotic, aztreonam, and other antibiotics on blood coagulation in vitamin K-deficient rats].

The influence of aztreonam (AZT), a new monobactam antibiotic, on blood coagulation was compared with latamoxef (LMOX), cefoperazon (CPZ), cefotetan (CTT) and ampicillin (ABPC). These antibiotics were administered intraperitoneally once a day for 7 days to rats fed a vitamin K-deficient diet. On the 8th day, blood coagulation activity and bacteria in the caecum were observed. 1) One hundred mg/kg and 300 mg/kg of LMOX prolonged the blood coagulation time and decreased normal prothrombin in a dose-dependent manner. CPZ, CTT and ABPC (300 mg/kg each) decreased both of these parameters, but not as much as LMOX did. AZT (300 mg/kg) had no effect on these parameters. 2) Three hundred mg/kg of ABPC and LMOX decreased the viable cell counts of all aerobic G (+), aerobic G (-), and anaerobic bacteria and yeast, while AZT decreased only aerobic G (-) bacteria. These results suggest that AZT may be less likely to induce hypoprothrombinemia than other antibiotics in clinical use.

Ampicillin↗
PubMed1987

[Comparative antibacterial activity of a new monobactam, carumonam (RO 17-2301, AMA 1080) on hospital bacteria resistant to beta lactams].

In vitro activity of a new monobactam, carumonam (RO 17-2301, AMA 1080) was tested against 370 hospital bacterial isolates. Results were compared to aztreonam, cefotaxime, cefmenoxime, latamoxef, ceftazidime, ceftriaxone, pefloxacin against Enterobacteriaceae, to aztreonam, piperacillin, cefoperazone, cefsulodin, ceftazidime, imipenem and pefloxacin against P. aeruginosa. All Enterobacteriaceae strains produced cephalosporinases and all P. aeruginosa strains were ticarcillin resistant. MIC 90% of carumonam against Enterobacteriaceae strains was lower than 0.25 mg/l for P. mirabilis, P. vulgaris, P. stuartii, Salmonella sp., ranged from 0.25 to 0.5 mg/l for Klebsiella sp. and S. marcescens, from 1 to 2 mg/l for E. coli and P. morganii, and from 4 to 8 mg/l for C. freundii and E. cloacae. The rate of strains inhibited with 4 mg/l of carumonam was 95.3%. So carumonam was at the second place from eight tested products, after latamoxef (97.5% of susceptible strains). Carumonam was active against second generation cephalosporins resistant strains when these strains were susceptible or intermediate to cefotaxime. Strains resistant to this compound escaped to its action. Its activity against A. calcoaceticus was weak (22.6% of strains inhibited by 4 mg/l), but was superior to that of cefsulodin against ticarcillin resistant P. aeruginosa strains (54.5 versus 16.1% of susceptible strains). However carumonam was less active against this last species than ceftazidime or imipenem (92.6 and 91% of susceptible strains respectively).

Anti-Bacterial Agents↗
PubMed2000

Cephalosporins, carbapenems, and monobactams.

Nonpenicillin beta-lactams exhibit a variable spectrum of antimicrobial activity, have a wide range of clinical uses and a favorable safety profile. Cefepime's twice-daily dosage and increased activity against Enterobacteriaceae may offer some advantages over older cephalosporins. The carbapenems offer a broad antimicrobial spectrum, and meropenem has an improved safety profile compared with imipenem. Aztreonam is a useful alternative for patients with aerobic gram-negative infections who are allergic to penicillin. The emergence of resistant organisms, however, is an increasing problem with the frequent use of these antibiotics.

Bacterial Infections↗
PubMed2000

PER-1 extended-spectrum beta-lactamase production in an Alcaligenes faecalis clinical isolate resistant to expanded-spectrum cephalosporins and monobactams from a hospital in Northern Italy.

An Alicaligenes faecalis (FL-424/98) resistant to expanded-spectrum cephalosporins and aztreonam was isolated from the urine of an inpatient at the Intensive Care Unit of the Varese Hospital (Northern Italy) after antimicrobial chemotherapy with cefazolin, vancomycin, and amikacin. Clavulanic acid restored the activity of expanded-spectrum cephalosporins, suggesting the production of an extended-spectrum beta-lactamase (ESbetaL). A crude extract of FL-424/98 showed the presence of two beta-lactamase activities focusing at pH 5.3 and 7.6, respectively. The ESbetaL activity, purified by means of three chromatographic steps, was found to correspond to the pI 5.3 enzyme. Determination of kinetic parameters confirmed that the enzyme efficiently hydrolyzed expanded-spectrum cephalosporins and aztreonam. A colony-blot hybridization revealed the presence of blaPER-related sequences in FL-424/98, and sequencing confirmed the identity of this determinant with blaPER-1, previously detected in Pseudomonas aeruginosa, Acinetobacter, and Salmonella clinical isolates from Turkey. Finding of blaPER-1 in a species that can be part of the resident human microbiota raises the possibility that it could be an efficient shuttle for spreading of this resistance gene among other opportunistic pathogens that are normally members of the resident microbiota. Kinetic parameters determined for the PER-1 enzyme with some cephalosporin substrates were somewhat different from those previously reported.

Adult↗
PubMed1986

In-vitro antibacterial activity of BO-1165, a new monobactam antibiotic.

BO-1165 has excellent antibacterial activity against Gram-negative bacteria but it is almost inactive against Gram-positive and anaerobic bacteria. BO-1165 was more active than the four reference drugs against Escherichia coli, Salmonella spp., Shigella spp., Klebsiella pneumoniae, Serratia marcescens, indole-positive and indole-negative Proteus. Also, BO-1165 exhibited high antibacterial activity against strains of Pseudomonas aeruginosa (MIC50, 3.12 mg/l) and P. cepacia (MIC50, 1.56 mg/l), but did not against Ps. maltophilia strains. BO-1165 had good stability to plasmid-mediated and chromosome-mediated beta-lactamases. However, the compound was slightly hydrolyzed by the beta-lactamases isolated from Proteus vulgaris, Ps. cepacia, Klebsiella oxytoca and Ps. maltophilia, which were capable of hydrolyzing aztreonam.

Aztreonam↗
PubMed1989

In-vitro activity of tigemonam, an oral monobactam, against gram-negative rods, including variants in beta-lactamase-production.

Tigemonam was compared in vitro with other orally active beta-lactams, aztreonam and ciprofloxacin against a selection of Gram-negative clinical isolates and laboratory-derived beta-lactamase-producing variants. Of the orally active beta-lactams, tigemonam was the most potent, with a spectrum of activity similar to that of aztreonam. This included stability to plasmid-mediated beta-lactamases and poor induction of chromosomal beta-lactamases. The susceptibility to Class I enzymes was only clinically significant for derepressed Enterobacter cloacae mutants. Tigemonam may have a valuable role in the management of infection caused by enterobacteria, particularly if bioavailability following oral administration is confirmed in human subjects.

Anti-Bacterial Agents↗
PubMed1988

In vitro antimicrobial activity of tigemonam, a new orally administered monobactam.

At five geographically separate medical centers, over 6,000 clinical bacterial isolates were tested for their susceptibility to tigemonam by the broth microdilution method. The antimicrobial spectrum of tigemonam was similar to that of aztreonam, but with two differences. Aztreonam was more active against Pseudomonas spp., and tigemonam was more active against some streptococci. Tigemonam was highly resistant to hydrolysis by the eight beta-lactamase enzymes tested. A significant (greater than a fourfold increase in the MICs of tigemonam) inoculum effect occurred when 3 of 13 isolates were tested with inocula of 5 X 10(5) and 1 X 10(7) CFU/ml. Tigemonam was bactericidal for all but 1 of the 13 isolates. Of the four quality-control strains recommended by the National Committee for Clinical Laboratory Standards, only Escherichia coli ATCC 25922 provided on-scale results. The proposed MIC quality-control range of tigemonam for E. coli ATCC 25922 is 0.13 to 0.5 micrograms/ml.

Aztreonam↗